Bergenin (compound of formula II), also known as dwarf tea, was first published in the “Plant Name Map,” which is a lactone formed by methyl gallic acid C-glucoside, usually white loose needle crystal or crystalline powder, and its plant source is mainly distributed in Yunnan, Sichuan, Tibet and other provinces in China. A large number of clinical trials have also confirmed that bergenin has anti-inflammatory analgesic, antitussive and antiasthmatic effects, and is often used as an effective component of cough and anti-inflammatory drugs in the treatment of cough, acute and chronic bronchitis, duodenal ulcer and the like. At present, bergenin tablets have been used as medicines for the treatment of chronic bronchitis. Recently, many pharmacological experiments have shown that bergenin has a variety of biological activities, including liver protection, anti-ulcer, improve immunity, anti-lipid oxidation and free radical scavenging. It was found that bergenin could effectively inhibit the lipid peroxidation stress in brain tissue after ischemia by inhibiting the increase of lipid peroxidation content in mouse brain tissue caused by ischemia/reperfusion injury. At the same time, the superoxide anion radical generated by the xanthine-xanthine oxidase system also has obvious scavenging effect. It is believed that bergenin has anti-lipid oxidation effect and it can be used as a new food additive for the production of vegetable oil to extend the shelf life of vegetable oil.
Thiodipropionic acid (cas: 111-17-1; compound of formula III) is a common antioxidant used in the industry to produce thioester antioxidants. A large number of studies shows that antioxidants are an important step in preventing aging, because free radicals or oxidants break down cells and tissues to affect metabolic functions, causing a variety of health problems. If excessive oxidative free radicals can be eliminated, many free radical-induced and aging-related diseases can be prevented.
In the present invention, structural modification of bergenin using thiodipropionic acid to obtain a sulfur-containing bergenin derivative. The antioxidant activity of the compound was verified by anti-oxidation experiments.